- |||||||||| lutetium Lu 177 rofapitide tetraxetan (AAA614) / Novartis
Journal: A preliminary study on the safety and efficacy of 177Lu-FAP-2286 in gastrointestinal tumours with positive FAP expression. (Pubmed Central) - Nov 7, 2025 These findings support the continued use of PARPi as maintenance therapy in biomarker-selected ovarian cancer populations, while promoting the need for individualized risk-benefit assessment and further research into resistance mechanisms and predictive biomarkers. 177Lu-FAP-2286 demonstrated good feasibility and safety in treating FAP-positive gastrointestinal tumors, resulting in disease stabilization in a subset of patients.
- |||||||||| PK/PD data, Preclinical, Journal: Preclinical Pharmacokinetics of DM5167, a Novel Selective PARP1 Inhibitor. (Pubmed Central) - Nov 6, 2025
DM5167 exhibited a favorable pharmacokinetic profile in vivo and in vitro. These findings support its potential for further clinical development and provide valuable insights to guide future preclinical and clinical studies of DM5167 and other PARP inhibitors.
- |||||||||| Review, Journal: Chimeric Antigen Receptor-Engineered (CAR)-T Cell Therapy for Metastatic Prostate Cancer. (Pubmed Central) - Oct 18, 2025
Furthermore, the introduction of poly (ADP-ribose) polymerase inhibitors like olaparib and rucaparib, has transformed the therapeutic landscape, particularly for patients with DNA repair deficiencies in metastatic prostate cancer...In this review, we highlight adoptive cellular therapies utilizing CAR-T cells engineered to recognize prostate cancer-specific antigens, aiming to overcome immune evasion mechanisms. We summarize current CAR-T modalities with their limitations and prospects being evaluated in both preclinical and clinical settings of metastatic prostate cancer.
- |||||||||| lucitanib (E 3810) / Clovis, Servier, vesencumab (MNRP1685A) / Roche, volociximab (M200) / AbbVie, Biogen
NephroAIX: Large Language Model (LLM)-Guided Knowledge Graph for Explainable Target Discovery in Human Kidney Diseases Using Single-Cell Data (Room 361A, Convention Center) - Oct 18, 2025 - Abstract #KIDNEYWEEK2025KIDNEY_WEEK_3439; For CKD, we found ATN-161, a peptide antagonist of integrin ?5?1, a receptor involved in cell-matrix adhesion, inflammation, and fibrosis, and VOLOCIXIMAB, a chimeric monoclonal antibody that targets integrin ?5?1 as two drugs associated with immune-podocyte interactions...Integrating AI with multi-modal single-cell omics holds immense potential to identify novel targets, elucidate disease pathways, and accelerate drug discovery. This synergy paves the way for precision nephrology, transforming how kidney diseases are understood and treated.
- |||||||||| Rubraca (rucaparib) / Pharma& Schweiz, apixaban / Generic mfg.
Journal: Rapid clearance of achiral small-molecule drugs using de novo-designed proteins and their cyclic and mirror-image variants. (Pubmed Central) - Oct 16, 2025 To assess the broader applicability of this approach, we extended our analysis to a de novo-designed protein targeting the anticancer drug rucaparib, further confirming its potential for small-molecule clearance. Our study shows that de novo-designed small-molecule-binding proteins can be used as antidotes in vivo, and that computational tools can be integrated with medicinal chemistry strategies for precise pharmacological interventions.
- |||||||||| Rubraca (rucaparib) / Pharma& Schweiz, Zejula (niraparib) / GSK, J&J
THE IMPACT OF PATHOGENIC VARIANTS OF BRCA1, BRCA2 AND OTHER DNA-REPAIR GENES ON THE SURVIVAL BENEFITS CONFERRED BY PARP INHIBITORS (E-Poster Stations) - Oct 15, 2025 - Abstract #IGCS2025IGCS_786; The median follow-up time was 27 months. Groups were balanced with respect to body mass index, proportions of patients with complete cytoreduction, stage at diagnosis, treatment setting, and PARPi treatment (Niraparib, Olarapib, and Rucaparib).
- |||||||||| Review, Journal, BRCA Biomarker, PARP Biomarker: The emerging role of PARP inhibitors in prostate cancer: A narrative review. (Pubmed Central) - Oct 13, 2025
While PARPi efficacy in BRCA-mutated mCRPC is well established, their role in earlier disease stages is currently under investigation. This non-systematic narrative review aims to summarize current evidence on PARPi in PC, outlining approved indications, ongoing clinical trials, and emerging therapeutic strategies across different disease settings.
- |||||||||| Rubraca (rucaparib) / Pharma& Schweiz, Lynparza (olaparib) / Merck (MSD), AstraZeneca
Review, Journal, PARP Biomarker: The interconnection between androgen receptor and DNA damage response pathways in prostate cancer. (Pubmed Central) - Oct 8, 2025 Consequently, recent preclinical and clinical studies have investigated combining AR-targeted therapies with treatments that induce DNA damage, such as radiation therapy, or inhibit DNA repair mechanisms. This review discusses AR's role in cellular processes, the interplay between AR and DDR, and recent advances in prostate cancer treatment strategies.
- |||||||||| Rubraca (rucaparib) / Pharma& Schweiz
Retrospective data, Journal: Receipt of PARP Inhibitors in Patients With Metastatic Prostate Cancer Harboring BRCA1/2 Alterations. (Pubmed Central) - Oct 2, 2025 Patients with mCRPC with evidence of harboring BRCA1/2 alterations and alive after August 15, 2020 (ie, 3 months after the approval of the first PARP inhibitor, rucaparib, in mCRPC) were included...This retrospective cohort study of patients with mCRPC and evidence of BRCA1/2 alterations found that approximately half of patients did not receive PARP inhibitors despite evidence of survival improvement in this population. These findings highlight the need to increase awareness of the survival data and access to life-prolonging therapies in patients with mCRPC.
- |||||||||| Beleodaq (belinostat) / Aurobindo, Assertio, Rubraca (rucaparib) / Pharma& Schweiz, alisertib (MLN8237) / Puma
Journal: Anti-cancer compound screening identifies Aurora Kinase A inhibition as a means to favor CRISPR/Cas9 gene correction over knock-out. (Pubmed Central) - Sep 26, 2025 The Aurora Kinase A inhibitor alisertib in particular led to an over 4-fold increase in preferential gene correction over gene knock-out in two cell models (HEK293T and Hepa 1-6) at sub-micromolar dosages on the eGFP locus, prompting further validation. On the long term this pathway did show cytotoxicity especially in the HEK293T cells, indicating further mechanistic investigation is needed, but this toxicity was less pronounced in primary hepatocytes.
- |||||||||| Rubraca (rucaparib) / Pharma& Schweiz
Journal: Rucaparib-Associated Drug Reaction With Eosinophilia and Systemic Symptoms Syndrome. (Pubmed Central) - Sep 22, 2025 We present a case of a 63-year-old woman who developed DRESS syndrome potentially after rucaparib and presented with fever, rash, eosinophilia, and elevated liver enzymes. The patient's symptoms resolved with systemic and topical steroids without any associated sequela.
- |||||||||| Rubraca (rucaparib) / Pharma& Schweiz
SAFETY OF RUCAPARIB MONOTHERAPY IN ADVANCED HIGH-GRADE OVARIAN CANCER CLINICAL TRIALS (Poster Area) - Sep 15, 2025 - Abstract #IGCS2025IGCS_470; 2019). In this updated integrated analysis of 1594 patients treated with rucaparib in all settings, the most frequent TEAEs were nausea, asthenia/fatigue/lethargy, and anemia/hemoglobin decreased with a median onset of 5, 15, and 57 days, respectively (Table 1).
- |||||||||| Lutathera (lutetium Lu 177 dotatate) / Novartis, Pluvicto (lutetium Lu 177 vipivotide tetraxetan) / Novartis, AAA614 / Novartis
Revisiting the Segmentation Threshold for Lu-177 SPECT (e-Poster Area) - Sep 12, 2025 - Abstract #EANM2025EANM_2533; In this updated integrated analysis of 1594 patients treated with rucaparib in all settings, the most frequent TEAEs were nausea, asthenia/fatigue/lethargy, and anemia/hemoglobin decreased with a median onset of 5, 15, and 57 days, respectively (Table 1). 1) Sphere-to-background ratios (SBRs): no background, 10:1, 5:1, 3.5:1 and 2:1 Phantom SPECT acquisitions Digital Jaszczak phantom 120 realistic noisy projections from SIMIND Monte Carlo simulation Physical Jaszczak phantom Dual-head NaI(Tl) SPECT system (Symbia T16, Siemens Healthineers, Germany) 120 projections, 25 s per view Fixed radius-of-rotation (ROR) of 24 cm 99m Tc imaging Primary energy window centered at 140 keV with a 15% window width (129.3-150.3 keV) A scatter window at 108.4-129.3 keV for the dual energy window scatter correction (SC) Low-energy high-resolution parallel hole collimators 177 Lu imaging Primary energy window centered at 208 keV with a 15% window width (192.4-223.6 keV) Two scatter windows at 161.2-192.4 keV and 223.6-244.4 keV for the triple energy window SC Medium energy general purpose parallel hole collimators Image reconstruction Filtered back projection (FBP) with Butterworth filter (cutoff frequency: 0.4, order 8 for 99m Tc; cutoff frequency: 0.4, order 5 for 177 Lu), SC and Chang
- |||||||||| Review, Journal, BRCA Biomarker, PARP Biomarker, IO biomarker: PARP Inhibitors in Genitourinary Cancer: A New Paradigm Beyond Prostate Cancer. (Pubmed Central) - Sep 4, 2025
More recently, pivotal clinical trials have broadened the potential of PARPis to the other GU cancers, including urothelial carcinoma and renal cell carcinoma. In this review, we examine the biomarkers for the response to PARPis beyond mutations in BRCA1/2 and discuss the current state and future perspectives of PARPis in GU cancers.
- |||||||||| Journal, BRCA Biomarker, PARP Biomarker: Identification of novel gene expression patterns and pathways involved in PARP-1 inhibitor resistance. (Pubmed Central) - Sep 4, 2025
KEGG Pathways "P53 signaling pathway" and "Positive regulation of developmental process(BP)", "endoplasmic reticulum lumen(CC)," and "growth factor binding(MF)", were found to be potentially associated with Olaparib resistance. Five hub genes were identified using PPI networking of which FN1, CCN2, and JUN may play a significant role in the development of Olaparib resistance and could be promising therapeutic and diagnostic biomarkers for dealing with Olaparib resistance in BRCA1/2 mutant breast and ovarian cancer.
- |||||||||| Rubraca (rucaparib) / Pharma& Schweiz, Lynparza (olaparib) / Merck (MSD), AstraZeneca, Zejula (niraparib) / GSK, J&J
Biomarker, Review, Journal, BRCA Biomarker, PARP Biomarker: Redefining Risk, Biomarkers, and Precision Therapy for Hereditary Ovarian Cancer: A Review. (Pubmed Central) - Sep 4, 2025 These agents significantly improved progression-free survival, establishing them as a cornerstone of precision oncology. This review delineates the evolving landscape of HOC, focusing on pharmacoepidemiology, risk assessment, chemoprevention, and targeted therapy, aiming to refine clinical decision-making and advance precision medicine for improved patient outcomes.
- |||||||||| Rubraca (rucaparib) / Pharma& Schweiz
Duodenal Ulcer Pathology: An Embryological Exploration (Exhibit Hall) - Aug 29, 2025 - Abstract #ACG2025ACG_4646; This review delineates the evolving landscape of HOC, focusing on pharmacoepidemiology, risk assessment, chemoprevention, and targeted therapy, aiming to refine clinical decision-making and advance precision medicine for improved patient outcomes. She had been lost to follow-up since 2022, after discontinuing rucaparib...She received IV pantoprazole and symptomatically improved, though her hemoglobin later dropped to 6.8 g/dL, requiring transfusion...Despite aggressive surgical debulking and peritoneal stripping, the patient developed late recurrence in the duodenum
- |||||||||| Rubraca (rucaparib) / Pharma& Schweiz, Lynparza (olaparib) / Merck (MSD), AstraZeneca, Zejula (niraparib) / GSK, J&J
Review, Journal, BRCA Biomarker, PARP Biomarker: From bench to bedside: Synthetic strategies and clinical application of PARP inhibitors. (Pubmed Central) - Aug 9, 2025 A provider advocacy approach is planned to improve response rates for the subsequent Phase 2 survey, in-depth interviews and focus group.prior to designing the Phase 3 pragmatic study Clinically approved inhibitors (olaparib, niraparib, rucaparib) demonstrate unprecedented efficacy, with olaparib extending median progression-free survival to 19.1
- |||||||||| tusamitamab ravtansine (SAR408701) / Sanofi, AbbVie, AAA614 / Novartis, BT5528 / Bicycle Therap
Review, Journal, IO biomarker: Innovative Peptide Therapeutics in the Pipeline: Transforming Cancer Detection and Treatment. (Pubmed Central) - Aug 2, 2025 By overcoming current limitations, peptide drugs are poised to redefine cancer management, offering safer, more effective alternatives to conventional therapies. Their integration into clinical practice could mark a critical milestone in achieving precision oncology.
- |||||||||| Preclinical evaluation of a 68 Ga/ 177 Lu theranostic targeting PARP for PARP-expressing cancers (Room 133+134) - Aug 1, 2025 - Abstract #EANM2025EANM_260;
Conclusion Taken together, we showed that KK02 selectively accumulates in tumor tissues while rapidly clearing from non-target healthy tissues. These findings highlight the strong potential of 68 Ga- and 177 Lu-labeled KK02 as a theranostic pair, allowing for the identification and personalized treatment of PARP-expressing cancers.
- |||||||||| Keytruda (pembrolizumab) / Merck (MSD), Rubraca (rucaparib) / Pharma& Schweiz
Trial completion date, Trial primary completion date: Rucaparib and Pembrolizumab for Maintenance Therapy in Stage IV Non-Squamous Non-Small Cell Lung Cancer (clinicaltrials.gov) - Jul 25, 2025 P1/2, N=25, Active, not recruiting, These findings highlight the strong potential of 68 Ga- and 177 Lu-labeled KK02 as a theranostic pair, allowing for the identification and personalized treatment of PARP-expressing cancers. Trial completion date: Jan 2028 --> Jun 2028 | Trial primary completion date: Jun 2025 --> Dec 2025
- |||||||||| KBD111 / Chengdu Baiyu Pharma
KBD111 is a highly selective, long-acting and brain-penetrant PARP1 inhibitor (Hall 25) - Jul 24, 2025 - Abstract #ESMO2025ESMO_4205; In an intracranial MDA-MB-436-luc model, KBD111 also demonstrated enhanced efficacy relative to AZD9574 under QW oral dosing...A phase 1 trial is planned for 2026. Legal entity responsible for the study The authors.
- |||||||||| Rubraca (rucaparib) / Pharma& Schweiz
5-year progression-free survival (PFS) with rucaparib (RUCA) maintenance in patients with newly diagnosed advanced ovarian cancer in ATHENA-MONO (GOG-3020/ENGOT-ov45) (Hall 25) - Jul 24, 2025 - Abstract #ESMO2025ESMO_2609; P3 There was a decreased risk of progression in all molecular subgroups, with the risk decreased by ?50% in the ITT, BRCA and HRD subgroups and ?40% and ?30% in the non-BRCA LOH high and non-BRCA LOH low subgroups, respectively. Incidence of MDS/AML remained low at 5 y. Table: 1073P Median investigator-assessed PFS, mo 5 y PFS rate, % RUCA PBO HR (95% CI) RUCA PBO ITT 20.2 9.2 0.53 (0.42-0.69) 29 16 HRD 31.4 12.0 0.52 (0.35-0.76) 37 22 BRCA 54.1 16.7 0.51 (0.29-0.90) 45 27 Non-BRCA LOH high 22.3 9.2 0.58 (0.35-0.96) 29 17 Non-BRCA LOH low 12.1 9.1 0.66 (0.46-0.95) 21 14 Non-BRCA LOH unknown 17.5 8.9 0.39 (0.20-0.77) 34 0 LOH, loss of heterozygosity
- |||||||||| Review, Journal, BRCA Biomarker, PARP Biomarker, IO biomarker: Synergistic strategies: ADC-PARP inhibitor combinations in triple-negative breast cancer therapy. (Pubmed Central) - Jul 20, 2025
Future directions include biomarker-driven patient selection, combination with immune checkpoint inhibitors, and advancement in next-generation ADCs. The synergistic potential of ADC-PARPi combinations provides a new avenue for overcoming TNBC resistance, enhancing treatment outcomes, and widening therapeutic strategies for this challenging disease.
- |||||||||| Xegafri (rociletinib) / Clovis
Journal: Covalent inhibition of ACSL4 alleviates ferroptosis-induced acute liver injury. (Pubmed Central) - Jul 19, 2025 Here, we identify Rociletinib (ROC) as a potent inhibitor of ferroptosis through virtual screening and mechanistic studies...ROC effectively mitigates ferroptosis-mediated acute liver injury in mouse models. These findings establish ROC as the targeted covalent inhibitor directly targeting ACSL4, offering a promising therapeutic strategy for ferroptosis-related diseases.
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